EP 3330264 B1 20200506 - PYRIDINE SUBSTITUTED 2-AMINOPYRIDINE PROTEIN KINASE INHIBITOR CRYSTAL
Title (en)
PYRIDINE SUBSTITUTED 2-AMINOPYRIDINE PROTEIN KINASE INHIBITOR CRYSTAL
Title (de)
PYRIDIN-SUBSTITUIERTER 2-AMINOPYRIDIN-PROTEINKINASE-INHIBITORKRISTALL
Title (fr)
CRYSTAL DE 2-AMINOPYRIDINE SUBSTITUÉ PAR LA PYRIDINE À ACTION INHIBITRICE DE PROTÉINE KINASES
Publication
Application
Priority
- CN 201510458524 A 20150730
- CN 2016092269 W 20160729
Abstract (en)
[origin: EP3330264A1] The present invention discloses a crystal of citrate salt of pyridine-substituted 2-aminopyridine-based protein kinase inhibitors, in particular, to crystal of 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4'-methoxy-6'-((S)-2-methylpiperazin -1-yl)-3,3'-bipyridin-6-amine citrate salt, a method for preparation thereof, a crystalline composition and a pharmaceutical composition comprising the crystal, and further discloses the use of crystals of citrate salt of the compound of Formula I in protein kinase-related diseases. The crystals of citrate salt according to the present invention are superior to 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4'-methoxy-6'-((S)-2-methylpiperazin-1-yl)-3,3'-bipyridin-6-amine or other salts of 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4'-methoxy-6'-((S)-2-methylpiperazin-1-yl)-3,3'-bipyridin-6-amine in at least one aspect of bioavailability, hygroscopicity, stability, solubility, purity, ease of preparation, and the like.
IPC 8 full level
C07D 401/14 (2006.01); A61K 31/496 (2006.01); A61P 35/00 (2006.01)
CPC (source: CN EP US)
A61K 31/496 (2013.01 - EP US); A61P 35/00 (2017.12 - EP US); C07D 401/14 (2013.01 - CN EP US); C07B 2200/13 (2013.01 - CN US)
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
DOCDB simple family (publication)
EP 3330264 A1 20180606; EP 3330264 A4 20190109; EP 3330264 B1 20200506; CN 107949560 A 20180420; CN 107949560 B 20190816; CN 110283161 A 20190927; CN 110283161 B 20210903; CN 110330483 A 20191015; DK 3330264 T3 20200602; HK 1250368 B 20200522; HU E050352 T2 20201130; JP 2018522067 A 20180809; JP 6513294 B2 20190515; TW 201704226 A 20170201; TW I707848 B 20201021; US 10385038 B2 20190820; US 2018244649 A1 20180830; WO 2017016514 A1 20170202
DOCDB simple family (application)
EP 16829879 A 20160729; CN 2016092269 W 20160729; CN 201680043892 A 20160729; CN 201910731904 A 20160729; CN 201910731905 A 20160729; DK 16829879 T 20160729; HK 18109836 A 20180731; HU E16829879 A 20160729; JP 2018524523 A 20160729; TW 105124294 A 20160801; US 201615749075 A 20160729